Sulfinpyrazone Aspirin

The hydrolysis of acetylsalicylic acid (aspirin) has also been described, and it involves the rapid acetylation of Lys199 [123], This reactive site also involves Trp214 and has been called the U-site [124], Drugs that inhibit the hydrolysis of substituted acetylsalicylic acids by HSA and decrease the fluorescence intensity of Trp214 are referred to as U-type drugs (e.g., sulfinpyrazone and warfarin). Because U-type drugs also bind to the site know as site I (which overlaps with subdomain IIA), the U-site and I-site are believed to overlap. Lysine residues also appear to be involved in the /3-lactamase activity of HSA [125],... 

Sulfinpyrazone is used in medicine as a nonsteroid anti-inflammatory, fever-reducing analgesic however, it is believed, that it inhibits cyclooxygenase of thrombocytes. In addition, it is also possible that its action is also linked with the action on membrane of thrombocytes and reduced quantities of secreted adenosine diphosphate and serotonin, which facilitate thrombocyte aggregation. Unlike aspirin, it has no effect on those who do not have irregular aggregation systems. 

Drugs that may be affected by aspirin include ACE inhibitors, acetazolamide, anticoagulants, anticonvulsants (hydantoins, valproic acid), beta blockers, diuretics, methotrexate, NSAIDs, oral hypoglycemics, and uricosuric agents (probenecid, sulfinpyrazone). 

Drugs that may affect aspirin include activated charcoal, ammonium chloride, ascorbic acid or methionine, antacids and urinary alkalinizers, carbonic anhydrase inhibitors, corticosteroids, and nizatidine. Drugs that may be affected by aspirin include alcohol, ACE inhibitors, anticoagulants (oral), beta-adrenergic blockers, heparin, loop diuretics, methotrexate, nitroglycerin, NSAIDs, probenecid and sulfinpyrazone, spironolactone, sulfonylureas and exogenous insulin, and valproic acid. 

Finally, sulfinpyrazone (Anturane) is usually administered to treat gouty arthritis, but has also shown some antithrombotic properties because of an ability to decrease platelet function. Sulfinpyrazone decreases platelet aggregation by inhibiting prostaglandin synthesis in a manner similar to aspirin. Sulfinpyrazone can be used as an alternative to aspirin in pre-... 

CaimsJA, Gent M, SingerJ, etal. Aspirin, sulfinpyrazone or both in unstable angina results of a Canadian multicenter trial. N Engl J Med 1985 313 1369-1375. 

A randomized trial of aspirin and sulfinpyrazone in threatened stroke. New England Journal of Medicine 299 53-59 CAPRIE Steering Committee (1996). 

ASPIRIN SULFINPYRAZONE High-dose aspirin antagonizes the urate-lowering effect of sulfinpyrazone Salicylates block sulfinpyrazone-induced inhibition of renal tubular reabsorption of urate Avoid long-term co-administration of high-dose aspirin with sulfinpyrazone. Low-dose aspirin does not seem to have this effect... 

Acetyl salicylic acid (aspirin). Nonsteroidal antiinflammatory dmp (NSADD), Phenylbutazone, Mdomethacin, Ibuprofen, Fenoprofen, Fluriboprofen, Neproxen, Sulfinpyrazone, antioxidants (Butylated Hydroxytoluene, BHT Butylated Hydroxyanisole, BHA Dipheylamine, DPA). 

Cairns JA, Gent M, Singer J, Finnie KJ, Froggdt GM, Holder DA, Jablcaisky G, Kostuk WJ, Melendez LJ, Myers MG Aspirin, sulfinpyrazone, or both in unstable angina Results of a Canadian multicenter trid. New Eng. J. Med. 212 1369,1985... 

Sulfinpyrazone can precipitate bronchoconstriction in some aspirin-sensitive patients (2). There is no cross-sensitivity with dipyrone. 

Szczekhk A, Czerniawska-Mysik G, Nizankowska E. Sulfinpyrazone and aspirin-induced asthma. N Engl J Med 1980 303(12) 702-3. 

In low dosages (up to 2g/day), aspirin reduces urate excretion and blocks the effects of sulfinpyrazone. In higher dosages (over 5g/day), salicylates increase urate excretion. 

Aspirin, sulfinpyrazone, and indomelhacin have an inliilii. lory effect on platelet aggregation. They inhibit cyckimy. genase. the enzyme that controls the formation of prosiaglan din endoperoxides and increases the tendency for ... 

Clinically important, potentially hazardous interactions with allopurinol, amiodarone, amobarbital, anabolic steroids, anti-thyroid agents, aprobarbital, aspirin, barbiturates, bivalirudin, butabarbital, butalbital, cimetidine, clofibrate, clopidogrel, cyclosporine, delavirdine, disulfiram, fenofibrate, fluconazole, gemfibrozil, glutethimide, imatinib, itraconazole, ketoconazole, levothyroxine, liothyronine, mephobarbital, methimazole, metronidazole, miconazole, penicillins, pentobarbital, phenobarbital, phenylbutazones, piperacillin, prednisone, primidone, propylthiouracil, quinidine, quinine, rifabutin, rifampin, rifapentine, rofecoxib, salicylates, secobarbital, sulfinpyrazone, sulfonamides, testosterone, thyroid, zileuton... 

The role of platelets in vascular disease, both on theoretical and clinical bases, has been discussed in many reviews.18-80 A report on ongoing clinical testing of aspirin and other inhibitors has also been summarized.81 Clinical results with several of the older inhibitors (aspirin, sulfinpyrazone, dipyridamole, etc.) have been reported,88... 

In the past 2 years progress has been rapid. Aspirin has proven to be effective in reducing the frequency of TIA. Sulfinpyrazone may reduce the death rate after MI. An inhibitor of platelet aggregation (BL 4162) developed specifically for this activity, and not already under evaluation or marketed for another indication, is being tested clinically. The future is indeed bright that some of these compounds will be useful in the control of thrombosis, which will stimulate further development of more potent and safer drugs and tools to enable us to understand the mechanisms involved in thrombosis and vascular disease. 

Nivaud-Guemet, E. Guemet, M. Ivanovic, D. Medenica, M. Effect of eluent pH on the ionic and molecular forms of the non-steroidal anti-inflammatory agents in reversed-phase high-performance liquid chromatography. J.Liq.Chromatogr, 1994, 17, 2343-2357 [also aspirin, flufenamic acid, keta-zone, mefenamic acid, niflumic, niflumic acid, nixylic acid, oxyphenbutazone, phenacetin, salicylamide, salicylic acid, sulfinpyrazone]... 

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